JP2018508491A5 - - Google Patents

Info

Publication number

JP2018508491A5

JP2018508491A5 JP2017540129A JP2017540129A JP2018508491A5 JP 2018508491 A5 JP2018508491 A5 JP 2018508491A5 JP 2017540129 A JP2017540129 A JP 2017540129A JP 2017540129 A JP2017540129 A JP 2017540129A JP 2018508491 A5 JP2018508491 A5 JP 2018508491A5

Authority

JP

Japan

Prior art keywords

oeg

γglu

pharmaceutical composition

human insulin

desb30 human

Prior art date

2015-01-29

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical class N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 45
• 239000008194 pharmaceutical composition Substances 0.000 claims description 25
• 102000004877 Insulin Human genes 0.000 claims description 22
• 108090001061 Insulin Proteins 0.000 claims description 22
• GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 11
• 229920005862 polyol Polymers 0.000 claims description 8
• 150000003077 polyols Chemical class 0.000 claims description 8
• 239000011780 sodium chloride Substances 0.000 claims description 7
• QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical group CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 6
• 239000000314 lubricant Substances 0.000 claims description 6
• 150000003839 salts Chemical class 0.000 claims description 6
• 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims description 5
• FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
• FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
• 239000000600 sorbitol Substances 0.000 claims description 4
• 235000021355 Stearic acid Nutrition 0.000 claims description 3
• 239000004026 insulin derivative Substances 0.000 claims description 3
• 239000008117 stearic acid Substances 0.000 claims description 3
• -1 medium chain fatty acid salt Chemical class 0.000 claims description 2
• 101700030984 B29K Proteins 0.000 claims 18
• 102200127556 GNPTAB K4Q Human genes 0.000 claims 10
• 239000004372 Polyvinyl alcohol Substances 0.000 claims 6
• 239000011248 coating agent Substances 0.000 claims 6
• 238000000576 coating method Methods 0.000 claims 6
• 229920002451 polyvinyl alcohol Polymers 0.000 claims 6
• 125000004432 carbon atoms Chemical group C* 0.000 claims 2
• 235000014113 dietary fatty acids Nutrition 0.000 claims 2
• 239000000194 fatty acid Substances 0.000 claims 2
• 150000004665 fatty acids Chemical class 0.000 claims 2
• 206010012601 Diabetes mellitus Diseases 0.000 claims 1
• 239000002775 capsule Substances 0.000 claims 1
• CTTKODQWVMTOPW-UHFFFAOYSA-N decanoic acid;sodium Chemical compound [Na].CCCCCCCCCC(O)=O CTTKODQWVMTOPW-UHFFFAOYSA-N 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 150000004667 medium chain fatty acids Chemical class 0.000 claims 1
• 239000000546 pharmaceutic aid Substances 0.000 claims 1
• KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
• 229910052708 sodium Inorganic materials 0.000 claims 1
• 239000011734 sodium Substances 0.000 claims 1
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
• 235000019359 magnesium stearate Nutrition 0.000 description 3
• QIQXTHQIDYTFRH-UHFFFAOYSA-M stearate Chemical compound CCCCCCCCCCCCCCCCCC([O-])=O QIQXTHQIDYTFRH-UHFFFAOYSA-M 0.000 description 3
• FBPFZTCFMRRESA-KAZBKCHUSA-N D-Mannitol Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KAZBKCHUSA-N 0.000 description 2
• FBPFZTCFMRRESA-KVTDHHQDSA-N Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
• 239000000594 mannitol Substances 0.000 description 2
• 235000010355 mannitol Nutrition 0.000 description 2
• 239000000203 mixture Substances 0.000 description 2
• DCXXMTOCNZCJGO-UHFFFAOYSA-N Stearin Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
• 239000002253 acid Substances 0.000 description 1
• 150000007513 acids Chemical class 0.000 description 1
• 239000008119 colloidal silica Substances 0.000 description 1
• VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1